Cytoskeletal Signaling

<p>2-Methylbutyrylcarnitine (chloride) acts as a gut microbial metabolite that targets integrin α2β1 on platelets, facilitating the activation of cytosolic phospholipase A2 (cPLA2) and enhancing platelet hyperresponsiveness. This compound further augments platelet hyperreactivity and promotes thrombus formation in mice. It is also characterized as a branched-chain acylcarnitine.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>Anti-GPRC5D Antibody is a humanized IgG1 monoclonal antibody targeting GPRC5D. It serves as the antibody component of the ADC molecule LM-305.</p>

<p>Alestramustine: a cancer drug that targets microtubules in estrogen receptor-positive cells, impeding cell division.</p>

<p>α-Linolenic acid (ALA) is an essential fatty acid found in leafy green vegetables.</p>

<p>Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. It is utilized in the synthesis of the diastereomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic diruthenium aqua complexes [Ru(Ph2phen)2(OH2)2]2+, offering integrin targeting and photoactivation properties. Consequently, Ac-MRGDH-NH2 can be applied in studies exploring tumor-targeted photoactivatable chemotherapy.</p>

<p>HSDVHK-NH2 TFA acts as an antagonist to the αvβ3-vitronectin integrin interaction, displaying an inhibitory concentration (IC 50) of 1.74 pg/mL (2.414 pM) [1] [</p>

<p>Ht-31 stearate: Blocks RII subunits of PKA &amp; AKAP interaction in cells; cell-permeable.</p>

<p>αVβ8-IN-1 is an αVβ8 integrin inhibitor that suppresses the growth of multiple tumour cell lines (EMT6, CT26, KPC, TKCC-10).</p>

<p>Microtubule-associated protein tau (26-44) is a synthetic peptide with an amino group conjugated to glutamine and a carboxyl group conjugated to lysine.</p>

<p>FRATtide inhibits the phosphorylation of Axin and β-catenin, inhibits GSK-3 binding to Axin, and is a peptide derived from the GSK-3 binding protein.</p>

<p>INY-03-041, a PROTAC pan-AKT degrader, targets AKT1/2/3 with IC50s: 2.0/6.8/3.5 nM; GDC-0068 + Lenalidomide fusion.</p>

<p>Tubulin polymerization-IN-78 (compound 10a) is an inhibitor of tubulin polymerization, with an IC50 value of 2.69 μM. It exhibits antiproliferative activity.</p>

<p>(8R)-8-Hydroxyepoxyboetirane A is a neuroactivating compound that interacts with PKCδ-C1B. This compound binds into the PKC enzyme pocket through hydrogen bonds with glycine-253, leucine-251, and threonine-242. It induces the release of NRG1 and promotes the differentiation of neural stem cells into neurons. (8R)-8-Hydroxyepoxyboetirane A holds potential for research into nervous system disorders.</p>

<p>Chaetominine is a type of cytotoxic alkaloid obtained from endophytic Chaetomium sp. IFB-E015.</p>

<p>Rotigaptide, modulates Cx43 for gap junctions, counteracts uncoupling, and maintains communication under stress.</p>

<p>Crosstide is a peptide analog of glycogen synthase kinase-3 (GSK-3) that functions as a natural substrate for Akt/PKB.</p>

<p>Pironetin, from Streptomyces, inhibits microtubule polymerization and tumor growth, and causes cell cycle arrest.</p>

<p>Aberrant tau degrader 2 (Compound 4-12) acts as a degrader of tau protein and serves as a target protein ligand for the synthesis of PROTAC degrader C004019.</p>

<p>Myokinasib-II acts as an inhibitor of MKLCK1.</p>

<p>MS133 is a human bispecific antibody targeting CD133/PROM1 and CD3E. It is used in the study of colon cancer.</p>

<p>hAChE-IN-1 (Compound 24) is a potent inhibitor of human acetylcholinesterase (hAChE), exhibiting an inhibition concentration half-maximum (IC50) of 1.09 μM.</p>

<p>Sudocetaxel is a compound that serves as a microtubule depolymerization inhibitor, specifically designed for the pH-sensitive delivery of docetaxel.</p>

<p>Betamethasone 17-benzoate is a representative steroid. It also can be used in the treatment of recurrent aphothous ulcers (RAU).</p>

<p>PKCδ Peptide Substrate is a highly specific substrate for the δ-type of Protein kinase C, composed of a sequence that mirrors murine eEF-1α (422-443) and</p>

<p>TPR proteins including CHIP, TPR1, and hSGT affect luciferase refolding by DnaJ and hsc70.</p>

<p>DSPE-PEG2000-iRGD is a PEG compound composed of DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrins and subsequently undergoes proteolytic cleavage within tumors, producing CRGDK/R, which interacts with neuropilin-1. This compound is characterized by its tumor-targeting and tumor-penetrating properties, making DSPE-PEG2000-iRGD suitable for drug delivery applications.</p>

<p>Zolbetuximab MMAE (IMAB362 MMAE) is a compound targeting Claudin 18.2 (CLDN18.2) with anti-cancer activity, used in the study of gastric and pancreatic cancers.</p>

<p>Fluc-IN-1 is a inhibitor of firefly luciferase (Fluc) and further inhibits WNT/β-catenin through Fluc without acting through Frizzled 7 or signaling amplifier.</p>

<p>Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.</p>

<p>para-amino-Blebbistatin is a water-soluble, stable, non-phototoxic inhibitor of non-muscle myosin II, with enhanced properties over blebbistatin.</p>

<p>Cys-McMMAF, a microtubule-disrupting agent linked to an anti-5T4 antibody, shows antitumor effects in mouse models.</p>

<p>Forimtamig (RG-6324) is a bispecific antibody that targets GPRC5D and CD3 T cells. It features a 2 + 1 structure, comprising two high-affinity GPRC5D binding segments and one CD3-binding module. Forimtamig is engineered with a P329G LALA mutation in its Fc domain to prevent Fcγ receptor and C1q binding, while maintaining Fc receptor interaction. Its isotype control corresponds to human IgG1 kappa.</p>

<p>G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.</p>

<p>Foxy-5 is a wnt5a peptide mimetic</p>

<p>DSPE-PEG2000-cRGD is a PEG compound composed of DSPE and an αvβ3-targeting peptide (cRGD). The cRGD peptide specifically binds to αvβ3 on the surface of various cancer cells and neovascular cells. This compound can be utilized for drug delivery.</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>MS5033 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades AKT (also known as protein kinase B), exhibiting a half-maximal degradation</p>

<p>DSPE-PEG3000-iRGD is a PEG compound comprising DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrin and undergoes proteolytic cleavage within tumors to produce CRGDK/R, interacting with neuropilin-1. This results in tumor targeting and penetration capabilities. DSPE-PEG3000-iRGD is applicable in drug delivery.</p>

<p>Delcasertib acetate is a selective δ protein kinase C (δPKC) inhibitor for the study of acute myocardial infarction and pain.</p>

<p>Anticanceragent 270 (Compound 8e) is a microtubule protein inhibitor with an IC50 of 1.02 μM against MCF-7 breast cancer cells. It exerts significant antiproliferative activity on breast cancer cells through a dual mechanism of inducing apoptosis and destabilizing microtubules. Anticanceragent 270 is useful for cancer research.</p>

<p>Larazotide: octapeptide from V. cholerae, treats Coeliac disease by inhibiting paracellular permeability.</p>

<p>ALB-109564 dihydrochloride: Semi-synthetic, vinblastine-derived, microtubule inhibitor, arrests tumor cells in G2/M phase.</p>

<p>Wnt pathway inhibitor 4 is a small molecule antimicrobial agent with antibacterial and antiproliferative activity against cancer cells.</p>

<p>hCA/Wnt/β-catenin-IN-1 (Compd 15) serves as an inhibitor with selective affinity for hCA isoforms II, IX, and XII, exhibiting K i values of 33.6, 24.1, and 6.8</p>

<p>Sangivamycin (NSC-65346) inhibits PKC (Ki=10μM) and hinders growth in various human cancers.</p>

<p>Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).</p>

<p>HA15-Biotin, a synthetic HA15-biotin conjugate, shows similar activity and may aid in proteomics.</p>

<p>SNIPER(ABL)-015, a compound that conjugates GNF5 (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 5</p>

<p>Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.</p>

<p>GRGDSPK TFA is an RGD peptide, competitive inhibitor of integrin-fibronectin, used to research integrins in bone dynamics.</p>

<p>MS98, a specific PROTAC AKT degrader, depletes T-AKT with DC50 of 78 nM; binds AKT1, AKT2, AKT3 with Kds of 4, 140, 8.1 nM.</p>

<p>Gantofiban is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist used in the treatment of cardiovascular disease and may be used to study thrombosis.</p>

<p>Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.</p>

<p>TBL-100 is a human monoclonal antibody (mAb) that targets Tau. It is applicable for research in Alzheimer's disease (AD) and progressive supranuclear palsy.</p>

<p>Dynamin IN-2 (compound 43) is a Wiskostatin analogue.</p>

<p>KIF18A-IN-2 is an inhibitor of mitotic kinesin Kif18A with IC50 of 28 nM and can be used in studies about chromosomal instability-associated vulnerabilities.</p>

<p>αvβ6-IN-2 (compound 20) is an effective orally active inhibitor of αvβ6 integrin (αvβ6integrin), with a pIC50 value of 7.8. It shows potential for use in research on idiopathic pulmonary fibrosis.</p>

<p>NSC 357754 dihydrochloride is an inhibitor of Claudin. It can enhance trans-epithelial electrical resistance and reduce the permeability of specific cations. This compound is useful for research into intestinal diseases mediated by Claudin-2 and/or Claudin-15.</p>

<p>Osemitamab (FUT8-KO) is a monoclonal antibody targeting claudin-18.2, expressed in CHO cells with a knockout of the fucosyltransferase 8 gene (FUT8). The absence of fucose heightens the antibody's ADCC effect. When combined with Capecitabine and Oxaliplatin, it can be used for G/GEJ cancer research.</p>

<p>Gly-Arg-Gly-Asp-Ser (GRGDS) GRGDS is a cell binding protein domain derived from the cell-binding region of fibronectin.</p>

<p>TAT-Gap19 TFA is a peptide that inhibits Cx43 hemichannels but not gap junctions and may reduce liver fibrosis.</p>

<p>Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).</p>

<p>Hsp110/sGC-modulator-1 (compound 17i) is a dual-target modulator of Hsp110 and sGC with oral activity, exhibiting optimal molecular activity against both Hsp110 and sGC targets. Additionally, it demonstrates significant inhibitory effects on malignant cellular phenotypes and vasodilation. Hsp110/sGC-modulator-1 (compound 17i) alleviates pulmonary vascular remodeling and right ventricular hypertrophy by inhibiting Hsp110.</p>

<p>Hsp90-IN-36 (compound 5) is an Hsp90 inhibitor with anticancer properties and exhibits an IC50 value of 14.74 μM against MCF-7 cells.</p>

<p>Myelin basic protein (MBP) is a protein believed to be important in the process of myelination of nerves in the nervous system.</p>

<p>LKKTETQ, a peptide segment within thymosin β 4, constitutes the protein's active site responsible for actin binding, cell migration, and wound healing.</p>

<p>KGDS is a synthetic peptide that targets the integrin GPIIb-IIIa on the membrane of activated human platelets, with the amino acid sequence Lys-Gly-Asp-Ser [1].</p>

<p>SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a</p>

<p>Alvespimycin (17-DMAG) TFA is a potent inhibitor of Hsp90, binding with an EC50 of 62 ± 29 nM.</p>

<p>fluorescent ligand that binds to the α4β1 integrin (VLA-4)</p>

<p>187-1, a cyclic 14-aa peptide, allosterically inhibits N-WASP, hindering actin assembly &amp; Arp2/3 activation with IC50 of 2 μM.</p>

<p>FF-21101 is a human IgG1 monoclonal antibody (mAb) that specifically targets CDH3/P-cadherin. It is suggested to use the isotype control, Human IgG1 kappa, for reference.</p>

<p>Certepetide, or iRGD, is a cyclic peptide that enhances tumor penetration and researches solid cancers.</p>

<p>Fuzapladib (IS-741) is a PLA2 inhibitor that reduces Mac-1 expression to prevent inflammation and pancreatitis.</p>

<p>Connexin43 peptide: lessens swelling, astrogliosis, inflammation, neuron death post-spinal injury; analgesic for neuropathic pain.</p>

<p>Tau/Aβ40 aggregation-IN-1 (Compound 20) functions as an inhibitor for tau and Aβ 40 aggregation, exhibiting IC50 values of 1.8 μM and 1.3 μM, respectively [1].</p>

<p>Inhibits N-WASP by stabilizing its autoinhibited form, blocking PIP2-induced actin assembly (IC50 ~2 μM), not directly affecting actin polymerization.</p>

<p>Ganodermaones B is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression .</p>

<p>Vinzolidine is a semi-synthetic vinca alkaloid. It exerts cytotoxic effects on tumor cells by inhibiting cell division through disruption of tubulin polymerization. Vinzolidine can be utilized in research to investigate synergy with other chemotherapy or biotherapy drugs, as well as cancer cell tolerance or resistance, and to explore strategies to overcome these challenges.</p>

<p>Tubulin Inhibitor 37 (Compound 12) effectively impedes tubulin aggregation (IC50 = 1.3 µM) and demonstrates antiproliferative activity against human tumor cell</p>

<p>17-DMAP-GA, a Geldanamycin analogue, acts as an HSP90 inhibitor, leading to cell cycle abnormalities.</p>

<p>Dynamin inhibitory peptide TFA hinders dynamin-amphiphysin interaction and endocytosis, affecting dopamine D3 and GABA A receptors.</p>

<p>Jatrophone is a novel inhibitor of the macrocyclic diterpenoid tumor.</p>

<p>Antitumor agent-190 (Compound 26) is a hexokinase 2 (Hexokinase2) inhibitor that exhibits significant antitumor activity by targeting both microtubules and hexokinase 2 (Hexokinase2), with an IC50 value of 0.764 μM against MD-MBA-231 cells. It effectively suppresses Hexokinase2 activity, resulting in the accumulation of reactive oxygen species (Reactive Oxygen Species) and disruption of mitochondrial membrane potential (MMP), thus promoting apoptosis and causing cell cycle arrest.</p>

<p>Tubulin inhibitor 24 is a potent inhibitor that can inhibit tubulin polymerization.</p>

<p>αvβ5 integrin-IN-1, a potent and selective αvβ5 integrin inhibitor, exhibits a high inhibitory potency with a pIC50 value of 8.2.</p>

<p>Tubulin polymerization-IN-48 (Compound 4k) is an inhibitor of tubulin polymerization, moderately disrupting the microtubule network.</p>

<p>Bimosiamose disodium (TBC-1269Z), a pan-selectin inhibitor, has IC50s: E-selectin 88 μM, P-selectin 20 μM, L-selectin 86 μM; anti-inflammatory.</p>

<p>HS-27 is a fluorescently-tethered inhibitor of Hsp90 with SNX-5422 tethered via a PEG linker to a fluorescein isothiocyanate or FITC.</p>

<p>Zolbetuximab (IMAB362) is a monoclonal antibody targeting Claudin-18.2 for certain gastrointestinal and pancreatic cancers.</p>

<p>β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI.</p>

<p>Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC).Bisindolylmaleimide III selectively interacts with PKCα or ribosomal S6</p>

<p>β-Catenin-IN-7 (Compound 9) is an inhibitor of β-catenin that disrupts its interaction with Tcf-4, consequently impeding Wnt-dependent gene expression, and</p>

<p>Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM.</p>

<p>SQLE-IN-1 is a SQLE inhibitor with antitumor activity that inhibits the proliferation of Huh7 and the protein expression of PI3K and AKT.</p>

<p>SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of</p>

<p>FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.</p>

<p>Myristoylated pep2m peptide; inhibits GluA2-NSF interaction, reducing AMPA receptor function and surface expression.</p>

<p>Gamitrinib TPP hexafluorophosphate is a mitochondrial-targeted HSP90 inhibitor with anticancer activity that can be used to study cancer and viral infection.</p>

<p>KQAGDV is a fibrinogen γ-chain cell adhesion peptide, targeting α2bβ3 integrin, and binds SMCs.</p>

<p>Anti-CDH17/Cadherin-17 Antibody (10C12) is a human-derived antibody produced in CHO cells, targeting CDH17. For isotype control, refer to HumanIgG1kappa, Isotype Control.</p>

<p>Fibronectin CS1 peptide inhibits tumor metastasis, lacking RGD domain; may aid cancer therapy.</p>

<p>AKT Kinase Inhibitor HCl is an Akt inhibitor with antitumor activity.</p>

<p>ML-B01 is an orally active inhibitor targeting Akt and PKA, with IC50 values of 2 nM and 136 nM, respectively. It demonstrates good blood-brain barrier (BBB) permeability in mice.</p>

<p>Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 28 - 62 mM).</p>

<p>RA-PR058 is an orally active Ramalin derivative capable of penetrating the blood-brain barrier, with multi-target regulatory functions. By reducing BACE1 expression, decreasing excessive tau protein phosphorylation, and mitigating anxiety-like behaviors, along with displaying favorable pharmacokinetic properties, RA-PR058 shows promise as a multi-target modulator for Alzheimer's disease.</p>

<p>PROTAC tubulin-Degrader-1 (Compound W13) functions as an inhibitor of PROTAC tubulin and exhibits anti-tumor activity against human lung cancer.</p>

<p>Cx43 blocker, IC50 ~7μM; doesn't affect gap junctions/Panx1. TAT motif enhances effect; works in vivo, brain-penetrant.</p>